The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Sep. 09, 1997
Filed:
Jan. 29, 1996
Applicant:
Inventors:
Norman A Abood, Morton Grove, IL (US);
Roger A Nosal, Buffalo Grove, IL (US);
Assignee:
G. D. Searle & Co., Chicago, IL (US);
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C / ; C07C / ;
U.S. Cl.
CPC ...
435280 ; 560 24 ; 560115 ; 560157 ;
Abstract
A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with .alpha.-chymotrypsin provides N-Boc-L-propargylglycine in high yield.